CHIR-99021 [252917-06-9]

Catalog number: HY-10182_5mg
Brand: MedChem Express
Packing: 5 mg
Other sizes: Other sizes available
Price: € 96.30
Expected delivery time: 10 days
CHIR-99021 Chemical Structure
CAS No. : 252917-06-9...

Product specifications for - CHIR-99021 [252917-06-9]

Product group: Chemicals
Category: Other
CAS No.: 252917-06-9
Purity: >98%
Molecular Formula: C22H18Cl2N8
Molecular weight: 465.34
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: CHIR-99021 (CT99021) is a GSK-3alpha/beta inhibitor with IC50 of 10 nM/6.7 nM, > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. IC50 value: 10 nM/6.7 nM for GSK-3alpha/beta [1] Target: GSK-3alpha/beta in vitro: CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 uM [1]. CHIR 99021 stabilizes free cytosolic beta-catenin and inhibits adipogenesis by blocking induction of CCAAT/enhancer-binding protein alpha and peroxisome proliferator-activated receptor gamma. Preadipocyte differentiation is inhibited when 3T3-L1 cells are exposed to CHIR 99021 for any 24 h period during the first 3 days of adipogenesis [2]. Unlike lithium chloride and AR-A014418, CHIR-99021 treatment does not reduce the viability of INS-1E cells even at high concentrations. Instead, CHIR-99021 robustly increases the rate of proliferation of INS-1E cells in a dose-dependent manner, and significantly inhibits INS-E cell death induced by high glucose and high palmitate in a concentration-dependent manner. CHIR-99021 promotes primary beta cell replication in isolated rat islets at concentrations as low as 1 uM, with 2-3 fold increase of cell replication at 5 uM of CHIR-99021 treatment [3]. in vivo: Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge [1]. Administration of CHIR-99021 significantly augments hematopoietic repopulation in recipient mice transplanted with mouse or human hematopoietic stem cells (HSCs), suggesting that GSK-3 is a specific modulator of HSC activity [3].
Safety information: 
Additional information: 
Synonyms: HY-10182; CT99021; MedChem Express
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